Highly Potent Phosphinic HIV‑1 Protease Inhibitors: Synthesis, In Vitro Evaluation, and Docking Studies.

ABSTRACT: In the search for effective HIV-1 protease inhibitors, the design of symmetrical phosphinic pseudopeptides derived from a dual addition of hypophosphorous acid to acrylates (PACs) has emerged as a promising strategy due to their nonhydrolyzable nature and high affinity for this protease. In this study, we report the synthesis, in vitro evaluation, and docking studies of a series of new symmetrical phosphinic inhibitors, synthesized via simple and cost-effective procedures. This approach overcomes the complexities of previous methods and utilizes commercially or readily available reagents. The synthesized PACs, featuring various P2 and P2' substituents, have been evaluated for their inhibitory activity against the HIV-1 protease. Among them, the PAC-Phe-Val derivative (

SUBMITTER: Hayat K 

PROVIDER: S-EPMC12750381 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature